inhibitory currents

By Targets:	Akt (1) Aldose Reductase (1) Calcium Channel (1) Endogenous Metabolite (2) ERK (1) GABA Receptor (3) Histamine Receptor (2) iGluR (1) JNK (1) mGluR (1) Oxytocin Receptor (1) Potassium Channel (3)
By Research Areas:	Cancer (1) Cardiovascular Disease (1) Endocrinology (1) Inflammation/Immunology (2) Metabolic Disease (1) Neurological Disease (11)
Click Chemistry:	Alkynes (1)

Targets Recommended: Macrophage migration inhibitory factor (MIF)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100372

E4CPG (RS)-ECPG	mGluR	Neurological Disease
E4CPG ((RS)-ECPG) is a Group I/Group II metabotropic glutamate receptor (mGluR) antagonist. E4CPG can inhibit the paired-pulse ratio of monosynaptic inhibitory postsynaptic currents (IPSC) potentiation .

HY-A0236A

Aprindine hydrochloride	Potassium Channel	Cardiovascular Disease
Aprindine hydrochloride is a class I-b anti-arrhythmic agent and a hERG channel blocker with an IC50 of 0.23 μM. Aprindine hydrochloride has inhibitory effects on Na+/Ca2+ exchanger currents, which is partly responsible for their antiarrhythmic and cardioprotective effects. Aprindine hydrochloride is widely used for trial and ventricular tachyarrhythmias research research.

HY-156061

NAP-1	GABA Receptor	Neurological Disease Inflammation/Immunology
NAP-1 is a compound with agent that can suppress or relieve pain. effects. NAP-1 enhances the inhibitory current by binding to a specific site of GABAaR, resulting in a narcotic effect. NAP-1 can be used in research to develop clinical agent that can suppress or relieve pain .

HY-106888A

CS-722	Endogenous Metabolite	Neurological Disease
CS-722 is a centrally acting muscle relaxant, and has a muscle relaxant activity and depressant effectson the spinal reflex[1]. CS-722 inhibits spontaneous inhibitory postsynaptic currents and excitatory postsynaptic currents in hippocampal cultures probably by an inhibition of both sodium and calcium currents .

HY-106888

CS-722 Free base	Endogenous Metabolite	Neurological Disease
CS-722 Free base is a synthesized centrally acting muscle relaxant, and has a muscle relaxant activity and depressant effectson the spinal reflex . CS-722 Free base inhibits spontaneous inhibitory postsynaptic currents and excitatory postsynaptic currents in hippocampal cultures probably by an inhibition of both sodium and calcium currents .

HY-135228

GZ4	Calcium Channel	Neurological Disease
GZ4 is a calcium current inhibitor with direct inhibitory activity on cell surface channels. GZ4 inhibition reverses mechanical hyperalgesia/hyperalgesia in a spinal nerve ligation-induced neuropathic pain model. The mechanism of action of GZ4 is similar to that of gabapentin, but the time course of its biological effects is more rapid, indicating that GZ4 can directly inhibit calcium channel currents .

HY-P4397

(d(CH2)51,Tyr(Me)2,Thr4,Orn8,des-Gly-NH29)-Vasotocin	Oxytocin Receptor	Endocrinology
(d(CH2)51,Tyr(Me)2,Thr4,Orn8,des-Gly-NH29)-Vasotocin, an oxytocin receptor antagonist, abolishes oxytocin-enhanced inhibitory postsynaptic currents in CA1 pyramidal neurons .

HY-161472

Aldose reductase-IN-7	Aldose Reductase	Cancer
Aldose reductase-IN-7 (Compound 6k) targets Aldose reductase. Aldose reductase-IN-7 exhibits potent enzyme inhibitory activity (K_i = 0.186 ± 0.020 μM), showing superiority to Epalrestat (HY-66009), which is currently in clinical use. Aldose reductase-IN-7 is less cytotoxic and possesses potent anticancer activity .

HY-108204

AZD 3043 THRX 918661	GABA Receptor	Others
AZD 3043 (THRX 918661) is a positive allosteric modulator of GABA(A) receptors with sedative and hypnotic activity. AZD 3043 can enhance GABA(A) receptor-mediated chloride currents in vitro and produce hypnotic and electroencephalographic inhibitory effects in vivo. Due to its esterase-dependent metabolic pathway, it has a short duration of action and can be quickly cleared even after long-term infusion, which may have clinical application potential.

HY-107717

MNI-caged-NMDA	iGluR	Neurological Disease
MNI-caged-NMDA is a light-sensitive amino acid with rapid release properties suitable for use in the study of fast synaptic receptor mechanisms. MNI-caged-NMDA shows metered release of NMDA receptors, inducing rapid and sustained receptor activation in cerebellar interneurons. MNI-caged-NMDA is able to achieve rapid transient responses and generate large inward currents by local laser photolysis. The use of MNI-caged-NMDA can effectively study neurotransmitter signaling and its inhibitory effects on GABA-A receptors .

HY-172140

Ebio3	Potassium Channel	Neurological Disease
Ebio3 is a selective potassium channel (KCNQ2) inhibitor with an IC₅₀ of 1.2 nM. Ebio3 binds to the KCNQ2 channel through its hydrophobic tail, causing the S6 helix to move inward, which leads to the closure of the inner gate. The inhibitory effect of Ebio3 is also effective in pathogenic mutants of KCNQ2 (such as R75C and I238L), where it can inhibit outward currents by more than 80%. Ebio3 is expected to be used in the research of neurological diseases such as epilepsy .

HY-135809

A2764 dihydrochloride	Potassium Channel	Neurological Disease
A2764 dihydrochloride is a highly selective inhibitor of TRESK (TWIK-related spinal cord K ⁺ channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC₅₀=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception .

HY-109968A

Irdabisant hydrochloride CEP-26401 hydrochloride	Histamine Receptor	Neurological Disease
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with K_i values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC₅₀ of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .

HY-109968

Irdabisant CEP-26401	Histamine Receptor	Neurological Disease
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with K_i values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC₅₀ of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .

HY-N7110

6-Hydroxyflavone	Akt ERK JNK GABA Receptor	Neurological Disease Metabolic Disease Inflammation/Immunology
6-Hydroxyflavone is an orally effective flavonoid compound. 6-Hydroxyflavone can inhibit LPS (HY-D1056) -induced NO production and has anti-inflammatory effects. 6-Hydroxyflavone promotes osteoblast differentiation by activating AKT, ERK 1/2 and JNK signaling pathways. 6-Hydroxyflavone has an inhibitory effect on bovine hemoglobin (BHb) glycosylation. 6-Hydroxyflavone has a kidney protective effect. In addition, 6-Hydroxyflavone enhances GABA-induced current through the Benzodiazepine sites of γ-aminobutyric acid (GABA_A) receptors. 6-Hydroxyflavone shows a clear preference for α2 - and α3 - subtypes, which play an anti-anxiety role .

Cat. No.	Product Name

HY-L118

Sodium Channel Blocker Library	153 compounds
Sodium channels conduct sodium ions (Na+) through a cell's plasma membrane that are the source of excitatory currents for the nervous system and muscle. Na channels are classified according to the trigger that opens the channel for such ions, i.e. either a voltage-change (Voltage-gated, voltage-sensitive, or voltage-dependent sodium channel also called VGSCs or Nav channel) or a binding of a substance (a ligand) to the channel (ligand-gated sodium channels). Dysfunction in voltage-gated sodium channels correlates with neurological and cardiac diseases, including epilepsy, myopathies, pain and cardiac arrhythmias. Sodium channel blockers are used in the treatment of cardiac arrhythmia, pain and convulsion. MCE offers a unique collection of 153 sodium channel blocker and antagonists, all of which have the identified inhibitory effect on sodium channels. MCE Sodium Channel Blocker Library can be used for neurological and cardiac diseases drug discovery and sodium channel research.

Sodium Channel Blocker Library

153 compounds

Sodium channels conduct sodium ions (Na+) through a cell's plasma membrane that are the source of excitatory currents for the nervous system and muscle. Na channels are classified according to the trigger that opens the channel for such ions, i.e. either a voltage-change (Voltage-gated, voltage-sensitive, or voltage-dependent sodium channel also called VGSCs or Nav channel) or a binding of a substance (a ligand) to the channel (ligand-gated sodium channels). Dysfunction in voltage-gated sodium channels correlates with neurological and cardiac diseases, including epilepsy, myopathies, pain and cardiac arrhythmias. Sodium channel blockers are used in the treatment of cardiac arrhythmia, pain and convulsion.

MCE offers a unique collection of 153 sodium channel blocker and antagonists, all of which have the identified inhibitory effect on sodium channels. MCE Sodium Channel Blocker Library can be used for neurological and cardiac diseases drug discovery and sodium channel research.

Cat. No.	Product Name	Target	Research Area

HY-P4397

(d(CH2)51,Tyr(Me)2,Thr4,Orn8,des-Gly-NH29)-Vasotocin	Oxytocin Receptor	Endocrinology
(d(CH2)51,Tyr(Me)2,Thr4,Orn8,des-Gly-NH29)-Vasotocin, an oxytocin receptor antagonist, abolishes oxytocin-enhanced inhibitory postsynaptic currents in CA1 pyramidal neurons .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N7110

6-Hydroxyflavone	Structural Classification Monophenols Flavonoids Classification of Application Fields Flavones Labiatae Source classification Phenols Plants Medicago truncatula Gaertn. Inflammation/Immunology Disease Research Fields	Akt ERK JNK GABA Receptor
6-Hydroxyflavone is an orally effective flavonoid compound. 6-Hydroxyflavone can inhibit LPS (HY-D1056) -induced NO production and has anti-inflammatory effects. 6-Hydroxyflavone promotes osteoblast differentiation by activating AKT, ERK 1/2 and JNK signaling pathways. 6-Hydroxyflavone has an inhibitory effect on bovine hemoglobin (BHb) glycosylation. 6-Hydroxyflavone has a kidney protective effect. In addition, 6-Hydroxyflavone enhances GABA-induced current through the Benzodiazepine sites of γ-aminobutyric acid (GABA_A) receptors. 6-Hydroxyflavone shows a clear preference for α2 - and α3 - subtypes, which play an anti-anxiety role .

HY-106888

CS-722 Free base	Structural Classification Natural Products Neurological Disease Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields	Endogenous Metabolite
CS-722 Free base is a synthesized centrally acting muscle relaxant, and has a muscle relaxant activity and depressant effectson the spinal reflex . CS-722 Free base inhibits spontaneous inhibitory postsynaptic currents and excitatory postsynaptic currents in hippocampal cultures probably by an inhibition of both sodium and calcium currents .

Cat. No.	Product Name		Classification

HY-172140

Ebio3		Alkynes
Ebio3 is a selective potassium channel (KCNQ2) inhibitor with an IC₅₀ of 1.2 nM. Ebio3 binds to the KCNQ2 channel through its hydrophobic tail, causing the S6 helix to move inward, which leads to the closure of the inner gate. The inhibitory effect of Ebio3 is also effective in pathogenic mutants of KCNQ2 (such as R75C and I238L), where it can inhibit outward currents by more than 80%. Ebio3 is expected to be used in the research of neurological diseases such as epilepsy .

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Click Chemistry